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Title: Illuminating phenylazopyridines to photoswitch metabotropic glutamate receptors: from the flask to the animals
Author: Gómez Santacana, Xavier
Pittolo, Silvia
Rovira, Xavier
López-Cano, Marc
Zussy, Charleine
Dalton, James A. R.
Faucherre, Adèle
Jopling, Chris
Pin, Jean-Philippe
Ciruela Alférez, Francisco
Goudet, Cyril
Giraldo, Jesús
Gorostiza Langa, Pablo Ignacio
Llebaria Soldevila, Amadeu
Keywords: Receptors de neurotransmissors
Neurotransmitter receptors
Issue Date: 25-Jan-2017
Publisher: American Chemical Society
Abstract: Phenylazopyridines are photoisomerizable compounds with high potential to control biological functions with light. We have obtained a series of phenylazopyridines with light dependent activity as negative allosteric modulators (NAM) of metabotropic glutamate receptor subtype 5 (mGlu5). Here we describe the factors needed to achieve an operational molecular photoisomerization and its effective translation into in vitro and in vivo receptor photoswitching, which includes zebrafish larva motility and the regulation of the antinociceptive effects in mice. The combination of light and some specific phenylazopyridine ligands displays atypical pharmacological profiles, including light-dependent receptor overactivation, which can be observed both in vitro and in vivo. Remarkably, the localized administration of light and a photoswitchable compound in the peripheral tissues of rodents or in the brain amygdalae results in an illumination-dependent analgesic effect. The results reveal a robust translation of the phenylazopyridine photoisomerization to a precise photoregulation of biological activity.
Note: Reproducció del document publicat a:
It is part of: ACS Central Science, 2017, vol. 3, num. 1, p. 81-91
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ISSN: 2374-7951
Appears in Collections:Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL))
Articles publicats en revistes (Ciència dels Materials i Química Física)
Articles publicats en revistes (Patologia i Terapèutica Experimental)

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